Tricyclic antidepressant drugs block histamine H2 receptor in brain

J. P. Green; S. Maayani

doi:10.1038/269163a0

Tricyclic antidepressant drugs block histamine H₂ receptor in brain

J. P. Green
, S. Maayani

Research output: Contribution to journal › Article › peer-review

185 Scopus citations

Abstract

THE observation that cyproheptadine is a competitive antagonist of the histamine H₂ receptor linked to adenylate cyclase in brain ¹ suggested that the chemically similar tricyclic antidepressant drugs may also have this activity. To test this hypothesis, four tricyclic antidepressants - representing four different structural types - were tested on the H₂ receptor linked to adenylate cyclase in homogenates of the guinea pig hippocampus and cortex. Both dimaprit and histamine were used as agonists. Dimaprit has potent activity at the H₂ receptor with negligible activity at the H₁ receptor, that is, less than 0.0001% of that of histamine².

Original language	English
Pages (from-to)	163-165
Number of pages	3
Journal	Nature
Volume	269
Issue number	5624
DOIs	https://doi.org/10.1038/269163a0
State	Published - 1977
Externally published	Yes

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title = "Tricyclic antidepressant drugs block histamine H2 receptor in brain",

abstract = "THE observation that cyproheptadine is a competitive antagonist of the histamine H2 receptor linked to adenylate cyclase in brain 1 suggested that the chemically similar tricyclic antidepressant drugs may also have this activity. To test this hypothesis, four tricyclic antidepressants - representing four different structural types - were tested on the H2 receptor linked to adenylate cyclase in homogenates of the guinea pig hippocampus and cortex. Both dimaprit and histamine were used as agonists. Dimaprit has potent activity at the H2 receptor with negligible activity at the H1 receptor, that is, less than 0.0001\% of that of histamine2.",

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AU - Green, J. P.

AU - Maayani, S.

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N2 - THE observation that cyproheptadine is a competitive antagonist of the histamine H2 receptor linked to adenylate cyclase in brain 1 suggested that the chemically similar tricyclic antidepressant drugs may also have this activity. To test this hypothesis, four tricyclic antidepressants - representing four different structural types - were tested on the H2 receptor linked to adenylate cyclase in homogenates of the guinea pig hippocampus and cortex. Both dimaprit and histamine were used as agonists. Dimaprit has potent activity at the H2 receptor with negligible activity at the H1 receptor, that is, less than 0.0001% of that of histamine2.

AB - THE observation that cyproheptadine is a competitive antagonist of the histamine H2 receptor linked to adenylate cyclase in brain 1 suggested that the chemically similar tricyclic antidepressant drugs may also have this activity. To test this hypothesis, four tricyclic antidepressants - representing four different structural types - were tested on the H2 receptor linked to adenylate cyclase in homogenates of the guinea pig hippocampus and cortex. Both dimaprit and histamine were used as agonists. Dimaprit has potent activity at the H2 receptor with negligible activity at the H1 receptor, that is, less than 0.0001% of that of histamine2.

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ER -

Tricyclic antidepressant drugs block histamine H2 receptor in brain

Abstract

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Tricyclic antidepressant drugs block histamine H₂ receptor in brain